Proteases
Proteases, also known as peptidases or proteolytic enzymes, consists of a large number of enzymes catalyzing the hydrolysis of peptide bonds and subsequently resulting in the degradation of protein substrates into amino acids. Proteases are involved in a wide range of human diseases, including cancer, neurodegenerative disorders, inflammatory diseases and cardiovascular diseases. Thus numerous proteases inhibitors (small molecules and proteins) have been identified to block activity of proteases. Proteases inhibitors can be classified into different types based on the class of proteases they inhibit through two general mechanisms, irreversible “trapping” reactions and reversible tight-binding reactions. Proteases inhibitors have been used as diagnostic or therapeutic agents for the treatment of proteases-related diseases.
- A4077 BIBR 953 (Dabigatran, Pradaxa)Summary: Thrombin inhibitor,potent,reversible and direct
- A4079 Fosinopril sodiumSummary: ACE inhibitor
- A4082 Olmesartan medoxomilSummary: AT1 receptor antagonist
- A4024 Danoprevir (RG7227)Target: HCV ProteasesSummary: HCV NS3/4A protease inhibitor
- A8204 LopinavirSummary: HIV protease inhibitor,highly potent
- A4031 Telaprevir (VX-950)Target: HCV NS3-4A proteaseSummary: HCV NS3-4A protease inhibitor
- A4032 VX-222 (VCH-222, Lomibuvir)Target: HCV polymeraseSummary: NNI of HCV RNA polymerase
- A4033 GlimepirideTarget: Inward Rectifier Potassium (Kir) ChannelsSummary: Sulfonylurea compound
- A4034 Linagliptin (BI-1356)Summary: DDP-4 inhibitor,highly potent and competitive
- A4036 Sitagliptin phosphate monohydrate5 CitationTarget: DPP-4Summary: Potent DPP-4 inhibitor